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    • 3. 发明授权
    • Azatyrosine analogues
    • 酪氨酸类似物
    • US5869507A
    • 1999-02-09
    • US899859
    • 1997-07-24
    • Hui-Po WangOn LeeJin-Yuh ShewShui-Jane Lee
    • Hui-Po WangOn LeeJin-Yuh ShewShui-Jane Lee
    • A61K31/44A61K31/4418A61P35/00C07D213/65
    • C07D213/65
    • A novel anti-oncogenic azatyrosine analogues of formula (I) ##STR1## wherein R.sub.1 is C.sub.1-6 alkyl, C.sub.1-6 haloalkyl, benzyl, or (C.sub.1-6 alkyl)carbonyl; R.sub.2 is C.sub.1-6 alkyl, C.sub.1-6 haloalkyl, or C.sub.1-6 alkoxyl; and R.sub.3 is CONR.sub.4 R.sub.5, CONHNR.sub.4 R.sub.5, or COOR.sub.6, wherein each R.sub.4 and R.sub.5 independently is a hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, or C.sub.3-6 cycloalkyl, or R.sub.4 and R.sub.5 taken together with the nitrogen attached thereto form a C.sub.3-8 heterocyclic group; R.sub.6 is C.sub.1-6 alkyl, C.sub.1-6 haloalkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or benzyl. Also disclosed is a method of preparing such a novel anti-oncogenic azatyrosine analogues, as well as a pharmaceutical composition containing a compound of formula (I).
    • 式(I)的新型抗致癌性酪氨酸类似物其中R 1为C 1-6烷基,C 1-6卤代烷基,苄基或(C 1-6烷基)羰基; R2是C1-6烷基,C1-6卤代烷基或C1-6烷氧基; 并且R 3是CONR 4 R 5,CONHR 4 R 5或COOR 6,其中每个R 4和R 5独立地是氢,C 1-6烷基,C 2-6烯基,C 2-6炔基或C 3-6环烷基,或者R 4和R 5与氮一起 附着其形成C 3-8杂环基; R 6是C 1-6烷基,C 1-6卤代烷基,C 2-6烯基,C 2-6炔基,C 3-6环烷基或苄基。 还公开了制备这种新型抗致癌性酪氨酸类似物的方法,以及含有式(I)化合物的药物组合物。
    • 5. 发明授权
    • Piperazinedione compounds
    • 哌嗪二酮化合物
    • US06635649B2
    • 2003-10-21
    • US09851077
    • 2001-05-08
    • Che-Ming TengHui-Po WangEric I. C. LiOn LeeJih-Hwa GuhHuei-Ting ChenYa-Bing FanYa-Lan Chen
    • Che-Ming TengHui-Po WangEric I. C. LiOn LeeJih-Hwa GuhHuei-Ting ChenYa-Bing FanYa-Lan Chen
    • A61K31496
    • C07D401/06C07D409/14
    • Piperazinedione compounds of the formula: Each of and and independently, is a single bond or a double bond; A is H or CH(RaRb) when is a single bond, or C(RaRb) when is a double bond; Z is R3O—(Ar)—B, in which B is CH(Rc) when is a single bond, or C(Rc) when is a double bond; Ar is heteroaryl; and R3 is H, alkyl, aryl, heteroaryl, C(O)Rd, C(O)ORd, C(O)NRdRe, or SO2Rd; each of R1 and R2, independently, is H, C(O)Rd, C(O)ORd, C(O)NRdRe, or SO2Rd; and each of Ra, Rb, Rc, Rd, and Re, independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl. Optionally, Ra and Rb taken together are cyclyl or heterocyclyl; and, also optionally, R1 and Ra or R1 and Rb taken together are cyclyl or heterocyclyl. Also disclosed is a method for treating tumor with the above described piperazinedione compounds.
    • 哌嗪二酮化合物,分别为:< CUSTOM-CHARACTER FILE =“US06635649-20031021-P00900.TIF”ALT =“custom character”HE =“20”WI =“20”ID =“CUSTOM-CHARACTER-00001”/ >和 或双键; 当是单键,或C(R a R b)当为双键时; 当是单键或C(R )”ALT =“自定义字符”HE =“20”WI =“20”ID =“CUSTOM-CHARACTER-00005”/>是双键; Ar是杂芳基; 且R 3为H,烷基,芳基,杂芳基,C(O)R d,C(O)OR d,C(O)NR d R e或SO 2 R d; R 1和R 2各自独立地是H,C(O)R d,C(O)OR d,C(O)NR d R e或SO 2 R ; R a,R b,R c,R d和R e各自独立地是H,烷基,芳基,杂芳基,环基或杂环基。 任选地,R 5和R b一起是环基或杂环基; 并且还可任选地,R 1和R 5'或R 1和R b一起是环基或杂环基。 还公开了用上述哌嗪二酮化合物治疗肿瘤的方法。